Publications & Patents

707. Synthesis of Functionalized Maoecrystal V Core Structures, K.C. Nicolaou, L. Dong, L. Deng, A.C. Talbot, D.Y.-K. Chen, Chem. Commun. 2010, 46, 70–72.

708. Cell Volume Decrease as a Link Between Azaspiracid-Induced Cytotoxicity and c-jun-N-Terminal Kinase Activation in Cultured Neurons, C. Vale, K.C. Nicolaou, M.O. Frederick, M.R. Vieytes, L.M. Botana, Toxicol. Sci. 2010, 113, 158–168.

709. Involvement of Capsase Activation in Azaspiracid-Induced Neurotoxicity in Neocortical Neurons, Z. Cao, K.T. Lepage, M.O. Frederick, K.C. Nicolaou, T.F. Murray, Toxicol. Sci. 2010, 214, 323–334.

710. Total Synthesis of (+)-Echinopines A and B, K.C. Nicolaou, H. Ding, J.-A. Richard, D.Y.-K. Chen, J. Am. Chem. Soc. 2010, 132, 3815–3118.

711. An Expedient Procedure for the Oxidative Cleavage of Olefinic Bonds with PhI(OAc)2, NMO, and Catalytic OsO4, K.C. Nicolaou, V.A. Adsool, C.R.H. Hale, Org. Lett. 2010, 12, 1552–1555.

712. Origins of Regioselectivity of Diels–Alder Reactions for the Synthesis of Bisanthraquinone Antibiotic BE-43472B, A.E. Haydon, J. Becker, Y.H. Lim, K.C. Nicolaou, K.N. Houk, J. Org. Chem. 2010, 75, 922–928.

713. Synthesis of the ABCDEFG Ring System of Maitotoxin, K.C. Nicolaou, R.J. Aversa, J. Jin, F. Rivas, J. Am. Chem. Soc. 2010, 132, 6855–6861.

714. Total Synthesis and Structural Revision of Vannusals A and B. Synthesis of the Originally Assigned Structure of Vannusal B, K.C. Nicolaou, A. Ortiz, H. Zhang, P. Dagneau, Lanver, A.; Jennings, M. P.; Arseniyadis, S.; Faraoni, R.; Lizos, D. E. J. Am. Chem. Soc. 2010, 132, 7138–7152.

715. Total Synthesis and Structural Revision of Vannusals A and B. Synthesis of the True Structures of Vannusals A and B, K.C. Nicolaou, A. Ortiz, H. Zhang, G. Guella, J. Am. Chem. Soc. 2010, 132, 7153–7176.

716. Total Synthesis and Biological Evaluation of the Resveratrol-Derived Polyphenol Natural Products Hopeanol and Hopeahainol A, K.C. Nicolaou, Q. Kang, T.R. Wu, C.S. Lim, D.Y.-K. Chen, J. Am. Chem. Soc. 2010, 132, 7540–7548.

717. Total Synthesis of Englerin A, K.C. Nicolaou, Q. Kang, S.Y. Ng, D.Y.-K. Chen, J. Am. Chem. Soc. 2010, 132, 8219–8222.

718. Total Synthesis and Structural Revision of Biyouyanagin B, K.C. Nicolaou, S. Sanchini, T.R. Wu, D. Sarlah, Chem. Eur. J. 2010, 16, 7678–7682.

719. Synthesis of the QRSTU Domain of Maitotoxin and Its 85-epi- and 86-epi-Diastereomers, K.C. Nicolaou, C.F. Gelin, J.H. Seo, Z. Huang, T. Umezawa, J. Am. Chem. Soc. 2010, 132, 9900–9907.

720. Asymmetric Total Synthesis of Cylindrocyclophanes A and F Through Cyclodimerization and a Ramberg–Bäcklund Reaction, K.C. Nicolaou, Y.-P. Sun, H. Korman, D. Sarlah, Angew. Chem. Int. Ed. 2010, 49, 5875–5878.

721. Total Synthesis of Sporolide B and 9-epi-Sporolide B, K.C. Nicolaou, J. Wang, Y. Tang, L. Botta, J. Am. Chem. Soc. 2010, 132, 11350–353.

722. Invigorating Education, K.C. Nicolaou, Angew. Chem. Int. Ed. 2011, 50, 63–74.

723. Synthesis of the C'D'E'F' Domain of Maitotoxin, K C. Nicolaou, J.H. Seo, T. Nakamura, R.J. Aversa, J. Am. Chem. Soc. 2011, 133, 214–219.

724. Synthesis of the WXYZA' Domain of Maitotoxin, K C. Nicolaou, T.M. Baker, T. Nakamura, J. Am. Chem. Soc. 2011, 133, 220–226.

725. Total Synthesis and Biological Evaluation of Monorhizopodin and 16-epi-Monorhizopodin, K.C. Nicolaou, X. Jiang, P.J. Lindsay-Scott, A. Corbu, S. Yamashiro, A. Bacconi, V.M. Fowler, Angew. Chem. Int. Ed. 2011, 50, 1139–1144.

726. Total Synthesis and Biological Evaluation of Marinopyrrole A and Analogs, K.C. Nicolaou, N.L. Simmons, J.S. Chen, N.M. Haste, V. Nizet, Tetrahedron Lett. 2011, 52, 2041–2043.

727. Maitotoxin: An Inspiration for Synthesis, K.C. Nicolaou, R.J. Aversa, Isr. J. Chem. 2011, 51, 359–377.

728. Design, Synthesis and Biological Evaluation of a Biyouyanagin Library, K.C. Nicolaou, S. Sanchini, D. Sarlah, G. Lu, D.K. Nomura, B.F. Cravatt, B. Cubitt, J.C. de la Torre, A.J. Hessell, D.R. Burton, Proc. Natl. Acad. Sci. U.S.A. 2011, 108, 6715–6720.

729. Addressing the Stereochemistry of Complex Organic Molecules by Density Functional Theory-NMR: Vannusal B in Retrospective, G. Saielli, K.C. Nicolaou, A. Ortiz, H. Zhang, A. Bagno, J. Am. Chem. Soc. 2011, 133, 6072–6077.

730. An Expedient Synthesis of a Functionalized Core Structure of Bielschowskysin, K.C. Nicolaou, V.A. Adsool, C.R.H. Hale, Angew. Chem. Int. Ed. 2011, 50, 5149–5152.

731. Enantioselective Dichlorinatoin of Allylic Alcohols, K.C. Nicolaou, N.L. Simmons, Y. Ying, P.M. Heretsch, J.S. Chen, J. Am. Chem. Soc. 2011, 133, 8134–8137.

732. Total Synthesis of Epicoccin G, K.C. Nicolaou, S. Totokotsopoulos, D. Giguère, Y. Sun, D. Sarlah, J. Am. Chem. Soc. 2011, 133, 8150–8153.

733. Proteomic Signature of Fatty Acid Biosynthesis Inhibition Available for In Vivo Mechanism of Action Studies, M. Wenzel, M Patra, D. Alrecht, D.Y.-K. Chen, K.C. Nicolaou, N. Metzler-Nolte, J.E. Bandow, Antimicrob. Agents Chemother. 2011, 55, 2590–2596.

734. Synthesis of the Carboline Disaccharide Domain of Shishijimicin A, K.C. Nicolaou, J.L. Kiappes, W. Tian, V.B. Gondi, J. Becker, Org. Lett. 2011, 13, 3924–3927.

735. Sulfonamides as a New Scaffold for Hypoxia Inducible Factor Pathway Inhibitors, C. Tan, R. de Noronha, N.S. Devi, A.A. Jabbar, S. Kaluz, Y.Liu, S. Reid Mooring, K.C. Nicolaou, B. Wang, E.G. Van Meir, Bioorg. Med. Chem. Lett. 2011, 21, 5528–5532.

736. Synthesis and Biological Evaluation of 2',4'- and 3',4'-Bridged Nucleoside Analogues, K.C. Nicolaou, S.P. Ellery, F. Rivas, K. Saye, E. Rogers, T.J. Workinger, M. Schallenberger, R. Tawatao, A. Montero, A. Hessell, F. Romesberg, D. Carson, D. Burton, Bioorg. Med. Chem. 2011, 19, 5648–5669.

737. Bioinspired Synthesis of Hirsutellones A, B and C, K.C. Nicolaou, Y.-P. Sun, D. Sarlah, W. Zhan, T.R. Wu, Org. Lett. 2011, 13, 5707–5710.

738. A Practical Sulfenylation of 2,5-Diketopiperazines, K.C. Nicolaou, D. Giguère, S. Totokotsopoulos, Y.-P. Sun, Angew. Chem. Int. Ed. 2012, 51, 728–732.

739. Synthesis of Macroheterocycles through Intramolecular Oxidative Coupling of Furanoid b-Ketoesters, K.C. Nicolaou, C.R.H. Hale, C. Ebner, C. Nilewski, C.F. Ahles, D. Rhoades, Angew. Chem. Int. Ed. 2012, 51, 4726–4730.

740. Bio-inspired Synthesis and Biological Evaluation of a Colchicine-related Compound Library, K.C. Nicolaou, R.A. Valiulin, J.K. Pokorski, V. Chang, J.S. Chen, Bioorg. Med. Chem. Lett. 2012, 22, 3776–3780.

741. Total Syntheses of Anominine and Tubingensin A, M. Bian, Z. Wang, X. Xiong, Y. Sun, C. Matera, K.C. Nicolaou, A. Li, J. Am. Chem. Soc. 2012, 134, 8078–8081.

742. Constructing Molecular Complexity and Diversity: Total Synthesis of Natural Products of Biological and Medicinal Importance, K.C. Nicolaou, C.R.H. Hale, C. Nilewski, H.A. Ioannidou, Chem. Soc. Rev. 2012, 41, 5185–5238.

743. A Total Synthesis Trilogy: Calicheamicin γ1I, Taxol, and Brevetoxin A, K.C. Nicolaou, C.R.H. Hale, C. Nilewski, Chem. Rec. 2012, 12, 407–441.

744. Aldehyde Dehydrogenase Inhibitors: A Comprehensive Review of the Pharmacology, Mechanism of Action, Substrate Specificity, and Clinical Application, V. Koppaka, D.C. Thompson, Y. Chen, M. Ellermann, K.C. Nicolaou, R.O. Juvonen, D. Petersen, R.A. Deitrich, T.D. Hurley, V. Vasiliou, Pharmacol. Rev. 2012, 64, 520–539.

745. Synthesis and Biological Evaluation of Epidithio-, Epitetrathio- and bis-(Methylthio)diketopiperazines: Synthetic Methodology, Enantioselective Total Synthesis of Epicoccin G, 8,8'-epi-ent-Rostratin B, Gliotoxin, Gliotoxin G, Emethallicin E and Haematocin and Discovery of New Antiviral and Antimalarial Agents, K.C. Nicolaou, M. Lu, S. Totokotsopoulos, P. Heretsch, D. Giguère, Y. Sun, D. Sarlah, T.H. Nguyen, I.C. Wolf, D.F. Smee, C.W. Day, S. Bopp, E.A. Winzeler, J. Am. Chem. Soc. 2012, 134, 17320–17332.

746. Arylsulfonamide KCN1 Inhibits In Vivo Glioma Growth and Interferes with HIF Signaling by Disrupting HIF-1α Interaction with Cofactors p300/CBP, S. Yin, S. Kaluz, N.S. Devi, A.A. Jabbar, R.G. de Noronha, J. Mun, Z. Zhang, P.R. Boreddy, W. Wang, Z. Wang, T. Abbruscato, Z. Chen, J.J. Olson, R. Zhang, M.M. Goodman, K.C. Nicolaou, E.G. Van Meir, Clin. Cancer Res. 2012, 18, 6623–6633.

747. How Thiostrepton Was Made in the Laboratory, K.C. Nicolaou, Angew. Chem. Int. Ed. 2012, 51, 12414–12436.

748. The Emergence of the Structure of the Molecule and the Art of Its Synthesis, K.C. Nicolaou, Angew. Chem. Int. Ed. 2013, 52, 131–146. Link to publication

749. General Synthetic Approach to Functionalized Dihydrooxepines, K.C. Nicolaou, R. Yu, L. Shi, Q. Cai, M. Lu, P. Heretsch, Org. Lett. 2013, 15, 1994–1997. Link to publication

750. Synthesis and Biological Evaluation of New Paclitaxel Analogs and Discovery of Potent Antitumor Agents, K.C. Nicolaou, R.A. Valiulin, Org. Biomol. Chem. 2013, 11, 4154–4163. Link to publication

751. Total Synthesis and Structural Revision of Viridicatumtoxin B, K. C. Nicolaou, C. Nilewski, C. R. H. Hale, H. A. Ioannidou, A. ElMarrouni, L. G. Koch, Angew. Chem. Int. Ed. 2013, 52, 8736–8741. Link to publication

752. Synthesis and Antioxidation Evaluation of (S,S)- (R,R)-Secoisolariciresinal Diglucosides (SDGs), O.P. Mishra, N. Simmons, S. Tyagi, R. Pietrofesa, V.V. Shuvaev, R.A. Valiulin, P. Heretsch, K.C. Nicolaou, M. Christofidou-Solomidou, Bioorg. Med. Chem. Lett. 2013, 23, 5325–5328. Link to publication

753. In Vivo Arrhythmogenicity of the Marine Biotoxin Azaspiracid-2 in Rats, S.F. Ferreiro, N. Vilariño, C. Carrera, M.C. Louzao, G. Santamarina, A.G. Cantalapiedra, L.P. Rodríguez, J.M. Cifuentes, A.C. Vieira, K.C. Nicolaou, M.O. Frederick, L.M. Botana, Arch. Toxicol. 2014, 88, 425–434. Link to publication

754. Microsphere-based Immunoassay for the Detection of Azaspiracids, L.P. Rodríguez, N. Vilariño, M.C. Louzao, T.J. Dickerson, K.C. Nicolaou, M.O. Frederick, L.M. Botana, Anal. Biochem. 2014, 447, 58–63. Link to publication

755. Cyclic Marinopyrrole Derivatives as Disruptors of Mcl-1 and Bcl-xL Binding to Bim, C. Cheng, Y. Liu, M. E. Balasis, N. L. Simmons, J. Li, H. Song, L. Pan, Y. Qin, K. C. Nicolaou, S. M. Sebti, R. Li, Mar. Drugs 2014, 12, 1335-1348. Link to publication

756. Organic Synthesis: The Art of Replicating the Molecules of Living Nature and Others Like Them in the Laboratory, K.C. Nicolaou, Proc. Royal Soc. A 2014, 470, 20130690. Link to publication

757. The Endeavor of Total Synthesis and Its Impact on Chemistry, Biology, and Medicine, K.C. Nicolaou, C.R.H. Hale, Natl. Sci. Rev. 2014, 1, 233-252. Link to publication

758. Marinopyrrole Derivatives with Sulfide Spacers as Selective Disruptors of Mcl-1 Binding to Pro-Apoptotic Protein Bim, C. Cheng, Y. Liu, M.E. Balasis, T.P. Garner, J. Li, N.L. Simmons, N. Berndt, H. Song, L. Pan, Y. Qin, K.C. Nicolaou, E. Gavathiotis, S.M. Sebti, R. Li. Mar. Drugs 2014, 12, 4311–4325. Link to publication

759. Advancing the Drug Discovery and Development Process, K.C. Nicolaou, Angew. Chem. Int. Ed. 2014, 53, 9128–9140. Link to publication

760. Total Synthesis of Viridicatumtoxin B and Analogues Thereof: Stretegy Evolution, Structural Revision, and Biological Evaluation, K.C. Nicolaou, C.R.H. Hale, C. Nilewski, H.A. Ioannidou, A. ElMarrouni, L.G. Nilewski, K. Beabout, T.T. Wang, Y. Shamoo, J. Am. Chem. Soc. 2014, 136, 12137–12160. Link to publication

761. Academic–Industrial Partnerships in Drug Discovery and Development, K.C. Nicolaou, Angew. Chem. Int. Ed. 2014, 53, 4730-4731. Link to publication

762. The Chemistry–Biology–Medicine Continuum and the Drug Discovery and Development Process in Academia, K.C. Nicolaou, Chem. Biol. 2014, 21, 1039–1045. Link to publication

763. Total Synthesis of Δ12-Prostaglandin J3, a Highly Potent and Selective Antileukemic Agent, K.C. Nicolaou, P. Heretsch, A. ElMarrouni, C.R.H. Hale, K.K. Pulukuri, A.K. Kudva, V. Narayan, K.S. Prabhu, Angew. Chem. Int. Ed. 2014, 53, 10443–10447. Link to publication

764. Total Synthesis of Myceliothermophins C, D and E, K.C. Nicolaou, L. Shi, M. Lu, M.R. Pattanayak, A.A. Shah, H.A. Ioannidou, M. Lamani, Angew. Chem. Int. Ed. 2014, 53, 10970–10974. Link to publication

765. Synthesis and Biological Evaluation of QRSTUVWXYZA′ Domains of Maitotoxin, K.C. Nicolaou, P. Heretsch, T. Nakamura, A. Rudo, M. Murata, K. Konoki, J. Am. Chem. Soc. 2014, 136, 16444–16451. Link to publication

766. In Vitro Chronic Effects on hERG Channel Caused by the Marine Biotoxin Azaspiracid-2, S.F. Ferreiro, N. Vilariño, M.C. Louzao, K.C. Nicolaou, M.O. Frederick, L.M. Botana, Toxicon 2014, 78, 69–75. Link to publication

767. Organic Synthesis, K.C. Nicolaou, C. Nilewski, in Discoveries in Modern Science: Exploration, Invention, Technology, J. Trefil, Ed., eBook, Macmillan Reference USA, MI, 2014. Link to publication

768. Total Synthesis of Trioxacarcin DC-45-A2, K.C. Nicolaou, Q. Cai, B. Qin, M.T. Peterson, R.J.T. Mikkelsen, P. Heretsch, Angew. Chem. Int. Ed. 2014, 53, in press. Link to publication

769. Synthesis and Biological Evaluation of Dimeric Furanoid Macroheterocycles: Discovery of New Anticancer Agents, K. C. Nicolaou, C. Nilewski, C. R. H. Hale, C. F. Ahles, C. A. Chiu, C. Ebner, A. ElMarrouni, L. Yang, K. Stiles, D. Nagrath, J. Am. Chem. Soc. 2015, 137, 4766–4770. Link to publication

770. Total Synthesis of Shishijimicin A, K. C. Nicolaou, Z. Lu, R. Li, J. R. Woods, T. Sohn, J. Am. Chem. Soc. 2015, 137 (27), 8716–8719. Link to publication

771. Total Synthesis and Structural Revision of Antibiotic CJ-16,264, K. C. Nicolaou, A. A. Shah, H. Korman, T. Khan, L. Shi, W. Worawalai, E. A. Theodorakis, Angew. Chem. Int. Ed. 2015, 54, 9203-9208. Link to publication

772. Practical Synthesis of p- and o-Amino- and Methoxyphenolic Anthraquinones, K. C. Nicolaou, M. Lu, P. Chen, and A. A. Shah, Angew. Chem. Int. Ed. 2015, 54, 12687-12691. Link to publication

773. Synthesis and Biological Evaluation of Novel Epothilone B Side Chain Analogues, K. C. Nicolaou, D. Rhoades, Y. Wang, S. Totokotsopoulos, R. Bai, E. Hamel, ChemMedChem 2015, 10, 1974–1979. Link to publication

774. Synthesis and Biopharmaceutical Evaluation of Imatinib Analogues Featuring Unusual Structural Motifs, K. C. Nicolaou, D. Vourloumis, S. Totokotsopoulos, A. Papakyriakou, H. Karsunky, H. Fernando, J. Gavrilyuk, D. Webb, A. F. Stepan, ChemMedChem 2016, 11, 31–37. Link to publication

775. Total Synthesis and Biological Evaluation of Natural and Designed Tubulysins, K. C. Nicolaou, D. Mandal, P. Klahn, J. Yin, M. Jin, R. D. Erande, J. Gavrilyuk, D. Vourloumis, J. Am. Chem. Soc. 2016, 138, 1698–1708. Link to publication

776. Total Synthesis of Trioxacarcins DC-45-A1, A, D, C and C7"-epi-C and Full Structural Assignment of Trioxacarcin C, K. C. Nicolaou, Q. Cai, H. Sun, B. Qin, S. Zhu, J. Am. Chem. Soc. 2016, 138, 3118–3124. Link to publication

777. Synthesis and Biological Investigation of Δ12-Prostaglandin J3 (12-PGJ3) Analogues and Related Compounds, K.C. Nicolaou, K.K. Pulukuri, S. Rigol, P. Heretsch, R. Yu, C.I. Grove, C.R.H. Hale, A. ElMarrouni, V. Fetz, M. Brönstrup, M. Aujay, J. Sandoval, J. Gavrilyuk, J. Am. Chem. Soc. 2016, 138, 6550–6560. Link to publication

778. Efficient Synthesis of Dimeric Oxazoles, Piperidines and Tetrahydroisoquinolines from N-Substituted 2-Oxazolones, Y. He, P.K. Agarwal, I.N. Chaithanya Kiran, R. Yu, B. Cao, C. Zou, X. Zhou, H. Xu, B. Xu, L. Zhu, Y. Lan, K.C. Nicolaou, Chem. Eur. J. 2016, 22, 7696–7701. Link to publication

779. Total Synthesis of Δ12-Prostaglandin J3 and Related Prostanoids: Evolution of Synthetic Strategies to a Streamlined Process, K.C. Nicolaou, K.K. Pulukuri, R. Yu, S. Rigol, P. Heretsch, C.I. Grove, C.R.H. Hale, A. ElMarrouni, Chem. Eur. J. 2016, 22, 8559–8570. Link to publication

780. Total Synthesis of Thailanstatin A, K.C. Nicolaou, D. Rhoades, M. Lamani, M.R. Pattanayak, S. Mothish Kumar, J. Am. Chem. Soc. 2016, 138, 7532–7535. Link to publication

781. Streamlined Total Synthesis of Uncialamycin and Its Application to the Synthesis of Designed Analogues for Biological Investigations, K.C. Nicolaou, Y. Wang, M. Lu, D. Mandal, M.R. Pattanayak, R. Yu, A.A. Shah, J.S. Chen, H. Zhang, J.J. Crawford, L. Pasunoori, Y.B. Poudel, N.S. Chowdari, C. Pan, A. Nazeer, S. Gangwar, G. Vite, E.N. Pitsinos, J. Am. Chem. Soc. 2016, 138, 8235–8246. Link to publication

782. Catalyst: Synthetic Organic Chemistry as a Force for Good, K.C. Nicolaou, Chem 2016, 1, 331–334. Link to publication

783. The Evolution and Impact of Total Synthesis on Chemistry, Biology and Medicine, K.C. Nicolaou, S. Rigol, Israel Journal of Chemistry 2017, doi: 10.1002/ijch.200201600087. Link to publication

784. Asymmetric Alkylation of Anthrones, Enantioselective Total Synthesis of (−)- and (+)-Viridicatumtoxins B and Analogues Thereof. Absolute Configuration and Potent Antibacterial Agents, K. C. Nicolaou, G. Liu, K. Beabout, M.D. McCurry, Y. Shamoo, J. Am. Chem. Soc. 2017, 2017, 139, 3736-3746. Link to publication

785. 12,13-Aziridinyl Epothilones. Stereoselective Synthesis of Trisubstituted Olefinic Bonds from Methyl Ketones and Heteroaromatic Phosphonates and Design, Synthesis, and Biological Evaluation of Potent Antitumor Agents, K.C. Nicolaou, D. Rhoades, Y. Wang, R. Bai, E. Hamel, M. Aujay, J. Sandoval, J. Gavrilyuk, J. Am. Chem. Soc. 2017, 139, 7318-7334. Link to publication

786. Experimental Evolution of Diverse Strains as a Method for the Determination of Biochemical Mechanisms of Action for Novel Pyrrolizidinone Antibiotics, K. Beabout, M. D. McCurry, H. Mehta, A. A. Shah, K. K. Pulukuri, S. Rigol, Y. Wang, K. C. Nicolaou, Y. Shamoo, ACS Infect Dis. 2017, 3, 854-865. Link to publication

787. Streamlined Total Synthesis of Trioxacarcins and Its Application to the Design, Synthesis and Biological Evaluation of Analogues Thereof. Discovery of Simpler Designed and Potent Trioxacarcin Analogues, K.C. Nicolaou, P. Chen, S. Zhu, Q. Cai, R. Erande, R. Li, H. Sun, K.K. Pulukuri, S. Rigol, M. Aujay, J. Sandoval, J. Gavrilyuk, J. Am. Chem. Soc. 2017, 139, 15467-15478. Link to publication

788. Enantioselective Total Synthesis of Antibiotic CJ-16,264, Synthesis and Biological Evaluation of Designed Analogues and Discovery of Highly Potent and Simpler Antibacterial Agents, K.C. Nicolaou, K.K. Pulukuri, S. Rigol, M. Buchman, A.A. Shah, N. Cen, M.D. McCurry, K. Beabout, Y. Shamoo, J. Am. Chem. Soc. 2017, 139, 15868-15877. Link to publication

789. Total Synthesis of Disorazoles A1 and B1 and Full Structural Elucidation of Disorazole B1, K.C. Nicolaou, G. Bellavance, M. Buchman, K.K. Pulukuri, J. Am. Chem. Soc. 2017, 139, 15636-15639. Link to publication

790. A brief history of antibiotics and select advances in their synthesis, K.C. Nicolaou, S. Rigol, The Journal of Antibiotics 2018, 71, 153-184. Link to publication

791. Improved Total Synthesis of Tubulysins and Design, Synthesis and Biological Evaluation of New Tubulysins with Highly Potent Cyto-toxicities Against Cancer Cells as Potential Payloads for Antibody-Drug Conjugates (ADCs), J. Am. Chem. Soc. 2018, 140, 3690-3711. Link to publication

792. The Emergence and Evolution of Organic Synthesis and Why It is Important to Sustain It as an Advancing Art and Science for Its Own Sake, K.C. Nicolaou, Isr. J. Chem 2018, 58, 104-113. Link to publication

793. Total Synthesis and Full Structural Assignment of Namenamicin, K.C. Nicolaou, R. Li, Z. Lu, E. Pitsinos, L.B. Alemany J. Am. Chem. Soc. 2018, 140, 8091-8095. Link to publication

794. Total Synthesis of Thailanstatins A−C, Spliceostatin D, and Analogues Thereof. Stereodivergent Synthesis of Tetrasubstituted Dihydro- and Tetrahydropyrans and Design, Synthesis, Biological Evaluation, and Discovery of Potent Antitumor Agents, K.C. Nicolaou, D. Rhoades, S.M. Kumar, J. Am. Chem. Soc. 2018, 140, 8303-8320. Link to publication

795. Streamlined Total Synthesis of Shishijimicin A and Its Application to the Design, Synthesis and Biological Evaluation of Analogues Thereof, and Practical Syntheses of PhthNSSMe and Related Sulfenylating Reagents, K.C. Nicolaou, R. Li, Z. Lu, E.N. Pitsinos, L.B. Alemany, M. Aujay, C. Lee, J. Sandoval, J. Gavrilyuk, J. Am. Chem. Soc. 2018, 140, 12120-12136. Link to publication

796. Syntheses of Cyclopropyl Analogues of Disorazoles A1 and B1 and Their Thiazole Counterparts, K.C. Nicolaou, M. Buchman, G. Bellavance, J. Krieger, P. Subramanian, K.K. Pulukuri, J. Org. Chem. 2018, 83, 12374-12389. Link to publication

797. Short Total Synthesis of Delta 12-Prostaglandin J2 and Related Prostaglandins. Design, Synthesis, and Biological Evaluation of Macrocyclic Delta 12-Prostaglandin J2 Analogues, K.C. Nicolaou, K.K. Pulukuri, S. Rigol, Z. Peitsinis, R. Yu, S. Kishigami, N. Cen, M. Aujay, J. Sandoval, N. Zepeda, J. Gavrilyuk, J. Org. Chem. 2019, 84, 365-378. Link to publication

798. Total Synthesis in Search of Potent Antibody–Drug Conjugate Payloads. From the Fundamentals to the Translational, K.C. Nicolaou, S. Rigol, Acc. Chem. Res. 2019, 52, 127-139. Link to publication

799. Total Synthesis Endeavors and Their Contributions to Science and Society: A Personal Account, K.C. Nicolaou, S. Rigol, R. Yu, CCS Chem. 2019, 1, 3-37. Link to publication

800. DNA Binding and Cleavage Modes of Shishijimicin A, K.C. Nicolaou, H. Zhang, R. Li, S. Ba, Z. Lu, E.N. Pitsinos, T. Li, J. Am. Chem. Soc. 2019, 141, 7842-7852. Link to publication

801. The Role of Organic Synthesis in the Emergence and Development of Antibody–Drug Conjugates as Targeted Cancer Therapies, K.C. Nicolaou, S. Rigol, Angew. Chem. 2019, 58, 11206-11241. Link to publication

802. Total Synthesis and Biological Evaluation of Tiancimycins A and B, Yangpumicin A, and Relatted Anthraquinone-Fused Enediyne Antitumor Antibiotics, K.C. Nicolaou, D. Das, Y. Lu, S. Rout, E.N. Pitsinos, J. Lyssikatos, A. Schammel, J. Sandoval, M. Hammond, M. Aujay, J. Gavrilyuk, J. Am. Chem. Soc. 2020, 142, 2549-2561. Link to publication

803. Design, Synthesis, and Biological Investigation of Epothilone B Analogues Featuring Lactone, Lactam, and Carbocyclic Macrocycles, Epoxide, Aziridine, and 1,1-Difluorocyclopropane and Other Fluorine Residues, K.C. Nicolaou, Y.G. Shelke, B.D. Dherange, A. Kempema, B. Lin, C. Gu, J. Sandoval, M. Hammond, M. Aujay, J. Gavrilyuk, J. Org. Chem. 2020, 85, 2865–2917 Link to publication

804. Perspectives from nearly five decades of total synthesis of natural products and their analogues for biology and medicine, K.C. Nicolaou, S. Rigol, Nat. Prod. Rep. 2020, 37, 1404-1435. Link to publication

805. Synthesis and Biological Evaluation of Shishijimicin A-Type Linker-Drugs and Antibody−Drug Conjugates, K. C. Nicolaou, R. Li, Q. Chen, Z. Lu, E. N. Pitsinos, A. Schammel, B. Lin, C. Gu, H. Sarvaiya, R. Tchelepi, A. Valdiosera, J. Clubb, N. Barbour, V. Sisodiya, J. Sandoval, C. Lee, M. Aujay, J. Gavrilyuk, J. Am. Chem. Soc. 2020, 142, 12890-12899. Link to publication

806. Streamlined Symmetrical Total Synthesis of Disorazole B1 and Design, Synthesis, and Biological Investigation of Disorazole Analogues, K. C. Nicolaou, J. Krieger, G. M. Murhade, P. Subramanian, B. D. Dherange, D. Vourloumis, S. Munneke, B. Lin, C. Gu, H. Sarvaiaya, J. Sandoval, Z. Zhang, M. Aujay, J. W. Purcell, J. Gavrilyuk, J. Am. Chem. Soc. 2020, 142 15476–15487. Link to publication

807. Total Synthesis of the Monomeric Unit of Lomaiviticin A, K.C. Nicolaou, Q. Chen, R. Li, Y. Anami, K. Tsuchikama, J. Am. Chem. Soc. 2020, 142, 20201-20207. Link to publication

808. Design, Synthesis, and Biological Investigation of Thailanstatin A and Spliceostatin D Analogues Containing Tetrahydropyran, Tetrahydrooxazine, and Fluorinated Structural Motifs, K.C. Nicolaou, S.R. Rekula, S.M. Mothish, A.R. Podilapu, R.P. Matuszak, P.M. Jung, L.T. Lam, A.C. Phillips, J. Lyssikatos, S. Munneke, C. Gu, H. Sarvaiya, J. Sandoval, M. Hammond, M. Aujay, J.W. Purcell, R.M. Reilly, J. Gavrilyuk, J. Org. Chem. 2021, 86, 2499-2521. Link to publication

809. Design, Synthesis, and Biological Evaluation of Tubulysin Analogues, Linker-Drugs, and Antibody–Drug Conjugates, Insights into Structure–Activity Relationships, and Tubulysin–Tubulin Binding Derived from X-ray Crystallographic Analysis, K.C. Nicolaou, S. Pan, K.K. Pulukuri, Q. Ye, S. Rigol, R.D. Erande, D. Vourloumis, B.P. Nocek, S. Munneke, J. Lyssikatos, A. Valdiosera, C. Gu, B. Lin, H. Sarvaiaya, J. Trinidad, J. Sandoval, C. Lee, M. Hammond, M. Aujay, N. Taylor, M. Pysz, J.W. Purcell, J. Gavrilyuk, J. Org. Chem. 2021, 86, 3377-3421. Link to publication

810. A Reverse Approach to the Total Synthesis of Halichondrin B, K. C. Nicolaou, S. Pan, Y. Shelke, D. Das, Q. Ye, Y. Lu, S. Sau, R. Bao, S. Rigol, J. Am. Chem. Soc. 2021, 143, 9267-9276. Link to publication

811. Uncialamycin-Based Antibody–Drug Conjugates: Unique Enediyne ADCs Exhibiting Bystander Killing Effect, K. C. Nicolaou, Stephan Rigol, Emmanuel N. Pitsinos, Dipendu Das, Yong Lu, Subhrajit Rout, Alexander W. Schammel, Dane Holte, Baiwei Lin, Christine Gu, Hetal Sarvaiya, Jose Trinidad, Nicole Barbour, Amanda M. Valdiosera, Joseph Sandoval, Christina Lee, Monette Aujay, Hanan Fernando, Anukriti Dhar, Holger Karsunky, Nicole Taylor, Marybeth Pysz, and Julia Gavrilyuk, Proc. Natl. Acad. Sci. U. S. A. 2021, 118, e2107042118. Link to publication

812. A Highly Convergent Total Synthesis of Norhalichondrin B, K. C. Nicolaou, S. Pan, Y. Shelke, Q. Ye, D. Das, and S. Rigol, J. Am. Chem. Soc. 2021, 143, 20970–20979. Link to publication

813. Total Synthesis of Gukulenin B via Sequential Tropolone Functionalizations, K. C. Nicolaou, R. Yu, Z. Lu, and F. G. Alvarez, J. Am. Chem. Soc. 2022, 144, 5190–5196. Link to publication

814. A Unified Strategy for the Total Syntheses of Eribulin and a Macrolactam Analogue of Halichondrin B, K. C. Nicolaou, S. Pan, Y. Shelke, S. Rigol, R. Bao, D. Das, Q. Ye, Proc. Natl. Acad. Sci. U.S.A. 2022, 119, e2208938119. Link to publication

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Publications

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1980–1989

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